WO2002045713A3 - Orally-bioavailable formulations of fentanyl and congeners thereof - Google Patents

Orally-bioavailable formulations of fentanyl and congeners thereof Download PDF

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Publication number
WO2002045713A3
WO2002045713A3 PCT/US2001/047651 US0147651W WO0245713A3 WO 2002045713 A3 WO2002045713 A3 WO 2002045713A3 US 0147651 W US0147651 W US 0147651W WO 0245713 A3 WO0245713 A3 WO 0245713A3
Authority
WO
WIPO (PCT)
Prior art keywords
congeners
fentanyl
orally
formulations
bioavailable formulations
Prior art date
Application number
PCT/US2001/047651
Other languages
French (fr)
Other versions
WO2002045713A2 (en
Inventor
Liming Shao
Original Assignee
Sepracor Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sepracor Inc filed Critical Sepracor Inc
Priority to AU2002241611A priority Critical patent/AU2002241611A1/en
Publication of WO2002045713A2 publication Critical patent/WO2002045713A2/en
Publication of WO2002045713A3 publication Critical patent/WO2002045713A3/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6949—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
    • A61K47/6951—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nanotechnology (AREA)
  • Biotechnology (AREA)
  • Biophysics (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Molecular Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

One aspect of the present invention relates to formulations of fentanyl and its congeners. A second aspect of the present invention relates to the use of the formulations of the present invention as analgesics in mammals.
PCT/US2001/047651 2000-12-04 2001-10-26 Orally-bioavailable formulations of fentanyl and congeners thereof WO2002045713A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002241611A AU2002241611A1 (en) 2000-12-04 2001-10-26 Orally-bioavailable formulations of fentanyl and congeners thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25114400P 2000-12-04 2000-12-04
US60/251,144 2000-12-04

Publications (2)

Publication Number Publication Date
WO2002045713A2 WO2002045713A2 (en) 2002-06-13
WO2002045713A3 true WO2002045713A3 (en) 2003-04-03

Family

ID=22950663

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/047651 WO2002045713A2 (en) 2000-12-04 2001-10-26 Orally-bioavailable formulations of fentanyl and congeners thereof

Country Status (3)

Country Link
US (1) US20020160991A1 (en)
AU (1) AU2002241611A1 (en)
WO (1) WO2002045713A2 (en)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030091629A1 (en) 1998-03-27 2003-05-15 Cima Labs Inc. Sublingual buccal effervescent
US6974590B2 (en) 1998-03-27 2005-12-13 Cima Labs Inc. Sublingual buccal effervescent
US6849263B2 (en) * 1998-12-21 2005-02-01 Generex Pharmaceutical Incorporated Pharmaceutical compositions for buccal delivery of pain relief medications
US20040224010A1 (en) * 2002-11-15 2004-11-11 Optime Therapeutics, Inc. Ophthalmic liposome compositions and uses thereof
US20040202717A1 (en) 2003-04-08 2004-10-14 Mehta Atul M. Abuse-resistant oral dosage forms and method of use thereof
JP5244318B2 (en) * 2003-12-31 2013-07-24 シーマ・ラブス、インコーポレイテッド Effervescent oral opiate dosage forms and methods of administration of opiates
WO2005065317A2 (en) * 2003-12-31 2005-07-21 Cima Labs Inc. Effervescent oral fentanyl dosage form
PT1708686E (en) * 2003-12-31 2011-04-20 Cima Labs Inc Generally linear effervescent oral fentanyl dosage form and methods of administering
US20070104763A1 (en) * 2005-11-10 2007-05-10 Navinta Llc Composition of fentanyl citrate oral solid transmucosal dosage form, excipient and binding material therefore, and methods of making
BRPI0707235B8 (en) * 2006-01-25 2021-05-25 Insys Therapeutics Inc sublingual fentanyl formulation without propellant, and, unit dose device for sublingual administration of a sublingual fentanyl formulation
PT103884A (en) * 2006-11-17 2008-05-19 Astrazeneca Ab PROLONGED RELEASE COMPOSITIONS AND METHODS FOR THEIR PREPARATION
US8173666B2 (en) 2007-03-12 2012-05-08 Nektar Therapeutics Oligomer-opioid agonist conjugates
US10512644B2 (en) 2007-03-12 2019-12-24 Inheris Pharmaceuticals, Inc. Oligomer-opioid agonist conjugates
US8486973B2 (en) 2007-08-02 2013-07-16 Insys Therapeutics, Inc. Sublingual fentanyl spray
EP2039360A1 (en) * 2007-09-19 2009-03-25 Euro-Celtique S.A. Non-invasive direct delivery of opioids to the central nervous system
US20140179615A1 (en) * 2012-07-12 2014-06-26 Hainan Weikang Pharmaceutical (Qianshan) Co., Ltd. Glutathione and Acetaminophen Composition and Preparation Method Thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992002256A1 (en) * 1990-08-01 1992-02-20 The Regents Of The University Of California Cyclodextrin complexes for neuraxial administration of drugs
US5451408A (en) * 1994-03-23 1995-09-19 Liposome Pain Management, Ltd. Pain management with liposome-encapsulated analgesic drugs

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1196033B (en) * 1984-02-22 1988-11-10 Chiesi Farma Spa COMPOUND WITH ANTI-INFLAMMATORY ACTIVITY OBTAINED BY COMPLEXATION WITH BETA-CYCLODEXTRINE AND RELATED PHARMACEUTICAL FORMULATIONS
US5231089A (en) * 1991-12-02 1993-07-27 University Of Florida Method of improving oral bioavailability of carbamazepine
DK0695169T3 (en) * 1993-04-22 2003-03-17 Skyepharma Inc Multivesicular liposomes with encapsulated cyclodextrin and pharmacologically active compounds and methods for using them
US6635661B2 (en) * 2000-05-25 2003-10-21 Sepracor Inc. Heterocyclic analgesic compounds and methods of use thereof
US6740639B1 (en) * 2000-03-29 2004-05-25 Council Of Scientific & Industrial Research Inclusion complees of a high potent opioid peptide, pharmaceutical compositions and method of treatment

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992002256A1 (en) * 1990-08-01 1992-02-20 The Regents Of The University Of California Cyclodextrin complexes for neuraxial administration of drugs
US5451408A (en) * 1994-03-23 1995-09-19 Liposome Pain Management, Ltd. Pain management with liposome-encapsulated analgesic drugs

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
DATABASE MEDLINE [online] 1990, MIKHAILOVA S ET AL: "[Liposomal systems--prospective drug forms. II. The creation and characterization of liposomal systems for the oral use of narcotic analgesics]", XP002208225, Database accession no. NLM1980460 *
EKSPERIMENTALNA MEDITSINA I MORFOLOGIIA. BULGARIA 1990, vol. 29, no. 3, 1990, pages 44 - 49, ISSN: 0367-0643 *
FARRAR J T ET AL: "ORAL TRANSMUCOSAL FENTANYL CITRATE: RANDOMIZED, DOUBLE-BLIND, PLACEBO-CONTROLLED TRIAL FOR TREATMENT OF BREAKTHROUGH PAIN IN CANCER PATIENTS", JOURNAL OF THE NATIONAL CANCER INSTITUTE, US DEPT. OF HEALTH, EDICATIONAND WELFARE, PUBLIC HEALTH, US, vol. 90, no. 8, 15 April 1998 (1998-04-15), pages 611 - 616, XP001058154, ISSN: 0027-8874 *
PORTENOY R K ET AL: "ORAL TRANSMUCOSAL FENTANYL CITRATE (OTFC) FOR THE TREATMENT OF BREAKTHROUGH PAIN IN CANCER PATIENTS: A CONTROLLED DOSE TITRATION STUDY", PAIN, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 2/3, no. 79, March 1999 (1999-03-01), pages 303 - 312, XP001076812, ISSN: 0304-3959 *
STANLEY T H ET AL: "ORAL TRANSMUCOSAL FENTANYL CITRATE (LOLLIPOP) PREMEDICATION IN HUMAN VOLUNTEERS", ANESTHESIA AND ANALGESIA, WILLIAMS AND WILKINS, BALTIMORE, MD, US, vol. 1, no. 69, July 1989 (1989-07-01), pages 21 - 27, XP008003100, ISSN: 0003-2999 *

Also Published As

Publication number Publication date
AU2002241611A1 (en) 2002-06-18
US20020160991A1 (en) 2002-10-31
WO2002045713A2 (en) 2002-06-13

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